The lethal dose is only 4-10x the effective dose, so it was a risk with the suicidal; also they have strong anticholingeric effects and made people uncomfortable. Anticholinergic effects also reduced cognition. The antihistamine in them caused sedation

Does imipramine have an approved use in children?

Yes, for bedwetting. Therefore imipramine was used for ADHD because it had a safety record in children. However, there is QT elongation and EKGs are required.

What two antidepressants combine effects on NE and serotonin?

Venlafaxine and duoloxetine (Effexor and Cymbalta)

Is Cymbalta approved for neuropathic pain?

yes

What is the advantage of a combination antidepressant?

It works on depression through two known pathways---NE leading to increased energy and concentration and Serotonin leading to reduced anxiety and depression.

a. What is the method of action of buproprion (Welbutrin

It is a DA transport blocker and weak NE blocker with little or no 5HT action

What are the uses of buproprion?

It avoids side effects of SSRIs and can add a new mechanism of action when added to SSRI. It is also used as an aid to quitting smoking

Who should avoid buproprion?

Individuals with seizure disorder and alcoholics (who could have seizures)

How do trazodone and mirtazapine work (Deseryl and Remeron)

Both of these increase serotonin through novel means (not by blocking reuptake). They can be used as adjuncts to SSRIs to boost serotonin. They also both have strong antihistamine actions so they are used to induce sleep

monoamine oxidase -an enzyme that decomposes serotonin, NE and dopamine in the neuron.

So inhibiting MAO does what?

Allows more NE, Serotonin,and DA to be reused, thus starting a cascade that can reduce depression and anxiety

Why are MAOI’s rarely used?

There is a risk for a fatal reaction if an individual eats certain hard cheese, hard sausages, or red wines that contain TYRAMINE. The dietary restrictions scare prescribers and patients

Is Lithium still a first line drug for mood stabilization?

Yes, it is quite effective but does cause tremor and diarrhea and weight gain

Why do we monitor Lithium levels?

Lithium is lethal in small overdose

Which other drug classes are used for mood stabilization?

The anticonvulsants that work on NA or CA channels or GABA reuptake, plus those that work to reduce glutamate. Most anticonvulsants affect cognition adversely and cause weight gain. Atypical antipsychotics are often used as monotherapies but concerns about metabolic syndrome are problematic.

Are the anticonvulsants FDA approved for mood stabilization?

Carbamazapine is in its long acting form called Equetro.

Which anticonvulsants have negative effects on cognition?

All have some negative effects on cognition. Phenobarbital and Topiramate may be the worst.

D2 receptor inhibition (in all DA pathways when we only want it in mesolimbic)

How are the atypicals different from the typicals?

They also inhibit Serotonin 2 receptors. The interaction between Serotonin and Dopamine allow more Dopamine in nirostriatal and tuberofundibular pathways and also in mesocortical pathway, which improves negative symptoms while still maintaining D2 blockage in mesolimbic

What causes Extra Pyramidal Symptoms?

DA/Ach imbalances in nigrostriatal pathways.

What is Tardive Dyskinesia-

a response to chronic DA blockade. Gait, limb, and buccal/tongue movements are affected. It is not always reversible when the medicine is discontinued.

What is Neuroleptic Malignant Syndrome?

A rare but potentially fatal reaction with hyperthermia, and muscle rigidity

What are side effects of typical antipsychotics?

Those with little Ach effect (like Haldol) can cause EPS. Almost all are sedating, reduce cognitive speed and cognitive efficiency

What are side effects of typical antipsychotics with Ach action (like Thorazine) –

cognitive blunting, constipation, hypotension, weight gain

What are side effects of atypicals?

Metabolic syndrome, increased risk for diabetes, stroke in the elderly

Which antipsychotic is recommended for Parkinson’s patients?

Quetiapine (seroquel)

What fatal side effect is associated with Clozapine?

Agranulocytosis

What method of administration is recommended for noncompliant psychotic patients?

Depot Haldol or Risperdal Consta

Do benzodiazapines aid cognition?

No, they reduce memory; some can be used to induce short term anterograde amnesia

b. What is the drug of choice for preventing seizures during alcohol withdrawal

Ativan, Serax or Librium

What is the method of action of benzodiazapines?

When GABA binds to a Chloride channel, stimultaneous binding of benzodiazepine will keep allow more Chloride to enter

What other substances bind to the same receptor?

Alcohol and Barbiturates

e. All benzodiazepines will cause physical dependence at regular doses within 2-8 weeks. TRUE or FALSE?

true

Which of these is not a form of methylphenidate?
Adderall
Metadate
Concerta
Straterra

Adderall and Straterra. Adderall is a mix of amphetamine. Straterra increases NE rather than focusing on DA. It is closer to a tricyclic antidepressant than to methylphenidate.